Fluticasone

Article Author:
Kailey Remien
Article Editor:
Andy Bowman
Updated:
5/10/2019 8:58:43 AM
PubMed Link:
Fluticasone

Indications

Fluticasone is corticosteroid given via oral, nasal, or topical routes. The route of administration depends on the patient’s diagnoses. Oral fluticasone is FDA-approved to treat asthma and has an off label use for chronic obstructive lung disease (COPD) and eosinophilic esophagitis. Inhaled steroids slightly improve lung function and improve symptoms of COPD but do not affect the rate of lung function decline.[1] Nasal fluticasone is used to treat allergic and non-allergic rhinitis, nasal polyps and allergies. The topical route treats atopic dermatitis and dermatoses.

Mechanism of Action

This drug is a corticosteroid and has a direct local effect of vasoconstriction and anti-inflammatory activity. Glucocorticoids inhibit the initial inflammatory events such as vasodilation, vascular permeability, and leukocyte emigration.[2][3] Fluticasone directly decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells. It reduces the number of these cells and also the number of cytokines they produce. This medication also directly increases beta-2 receptors on airway smooth muscle and decreases mucus gland secretions.[3] This corticosteroid also increases the anti-inflammatory effects of annexin-1, secretory leukoprotease inhibitor (SLPI), mitogen-activated kinase phosphatase-1 (MKP-1), glucocorticoid-induced leucine zipper protein (GILZ), and I-kappa B-alpha and inhibitor of NF-kappa B.[3] 

Administration

Oral – the oral medication can be given via a dry powder inhaler, a metered dose inhaler or a swallowed form. The dry powder should be administered at roughly the same time daily, and after inhalation, the patient should rinse their mouth and spit out the water to avoid oral thrush. To accurately receive the medication from the metered inhaler one should shake the canister and spray upon inhalation. No spacer should be used for the dry powder but is an option for the metered dose inhaler. The swallowed form, only for eosinophilic esophagitis, will be sprayed into the pharynx and swallowed. The patient should not eat or drink for the next 30 minutes following administration.

Patients who take fluticasone have a higher incidence of oral thrush than those taking beclomethasone.[4] This increase has a positive relationship with dosage, as Candida spp. infection increases as fluticasone amount increases. Gargling with amphotericin B is an effective treatment for fluticasone associated thrush.[4] 

Nasal – the nasal spray is to be used at regular intervals and is not to be sprayed in the mouth or eyes. Shake the bottle gently before each use. While keeping the bottle upright, plug one nostril and press pump to release spray into the other nostril. During the spraying of the medication, the patient should take a deep inhalation through the nose.

Topical – apply a thin layer and rub into skin. Avoid contact with eyes, and this medication should not be used on the face, armpits or groin unless directed otherwise.

Adverse Effects

Local[3]: 

  • Dysphonia
  • Oropharyngeal candidiasis
  • Cough
  • Pneumonia

Between 10 and 20% of inhaled corticosteroids make it to the lungs, which means 80 to 90% go through to GI tract. The liver inactivates much of the medication during its first pass, and the amount of drug not inactivated by the liver and those absorbed in the lungs is what is responsible for the systemic effects.[3] 

Systemic[3]:

  • Adrenal suppression
  • Growth suppression
  • Bruising
  • Osteoporosis
  • Cataracts
  • Glaucoma
  • Metabolic abnormalities
  • Psychiatric disturbances

It has been found, in asthmatic patients, there is a 21% higher risk of a severe asthma exacerbation when treated with fluticasone alone when compared to those treated with a combination of fluticasone and salmeterol.[5]

Contraindications

Hypersensitivity to the medication. Many formulations contain milk proteins or lactose and those with known allergies to these substances should not use this medication.[6]

Fluticasone is contraindicated as a primary treatment of acute bronchospasm.[7]

Monitoring

Patients on fluticasone should undergo monitoring for the adverse effects listed above. The practitioner should ask the patient about cough, recent illnesses, bruising, changes to their mood and vision disturbances. Providers should monitor for signs of hippocampus-pituitary-adrenal axis suppression, and oral candidiasis. PFTs and DEXA scans may be useful in patients with complaints associated with new breathing changing and signs of osteoporosis.

 Slowed growth in children and reduced mineral density are problematic effects of inhaled corticosteroids. Studies show that the decreased growth was permanent in children who used budesonide but those who used fluticasone the effect was long-lasting but potentially not permanent.[8] Decreased bone density in children was only associated with high dose, inhaled corticosteroids (ICS). Children’s growth should be monitored every 3 to 6 months and those taking high dose ICS should have their bone mineral density monitored yearly.[8] 

Toxicity

There is documentation of substantial lactic acidosis after an overdose of inhaled salmeterol and fluticasone.[9] The patient has inhaled 60 puffs of the combination medication in a suicide attempt and presented with a sympathomimetic syndrome, metabolic acidosis, and hyperlactatemia. SHe received supportive therapy, and she was within normal health limits the following day.[9] This clinical presentation was likely due to the salmeterol more so than the fluticasone and lends support to the idea that fluticasone is a relatively safe medication.

Enhancing Healthcare Team Outcomes

Inhaled corticosteroids have been found to cross the placenta. However, research has found no significant association between ICS and congenital organ malformations.[10] There have been documented risk to the fetus with maternal asthma exacerbations. The risk-benefit ratio should be a consideration when prescribing ICS to pregnant women.[10]

A 6-month observational study found that elderly patients had a sustained improved knowledge and use of inhalers when educated by an on-staff pharmacist.[11] Optimizing user technique ultimately provides them with the most medication possible per administration. They are more likely to receive benefits and symptom resolution and less likely to change medications when receiving their prescribed dose. Working with pharmacists to provide new and old inhaler users with administration techniques will increase their medication satisfaction and their health outcomes.[11]

Another study assessed the effect of pretreatment with fluticasone for 6 weeks before seasonal allergen provocation; this was a double-blind, placebo-controlled study. They found that after 4 weeks of treatment with 200mg of fluticasone twice daily there were significant histologic changes.[12] There were fewer epithelial Langerhans cells, mast cells, T cells, macrophages, and eosinophils in the nasal mucosa of those who received fluticasone when compared to the placebo group. Cellular influx after allergen exposure was also significantly decreased in this group after 4 weeks of treatment. Fluticasone was found to be effective in early and late phase allergic rhinitis.[12] Healthcare practitioners should advise prompt prophylactic treatment with fluticasone for their patients with allergic nasal symptoms.

Since fluticasone is now available in the USA as an over the counter medication, health practitioners should work in an interprofessional team to ensure compliance and proper use; this collaborative team approach includes physicians, nurses, and pharmacists, communicating across disciplines to ensure optimal therapeutic outcomes while minimizing adverse effects and patient risk. [Level V]


References

[1] Noseda A, [Drug therapies of COPD]. Revue medicale de Bruxelles. 2003 Sep;     [PubMed PMID: 14606301]
[2] Coutinho AE,Chapman KE, The anti-inflammatory and immunosuppressive effects of glucocorticoids, recent developments and mechanistic insights. Molecular and cellular endocrinology. 2011 Mar 15;     [PubMed PMID: 20398732]
[3] Barnes PJ, Inhaled Corticosteroids. Pharmaceuticals (Basel, Switzerland). 2010 Mar 8;     [PubMed PMID: 27713266]
[4] Fukushima C,Matsuse H,Tomari S,Obase Y,Miyazaki Y,Shimoda T,Kohno S, Oral candidiasis associated with inhaled corticosteroid use: comparison of fluticasone and beclomethasone. Annals of allergy, asthma     [PubMed PMID: 12839324]
[5] Stempel DA,Raphiou IH,Kral KM,Yeakey AM,Emmett AH,Prazma CM,Buaron KS,Pascoe SJ, Serious Asthma Events with Fluticasone plus Salmeterol versus Fluticasone Alone. The New England journal of medicine. 2016 May 12;     [PubMed PMID: 26949137]
[6] Robles J,Motheral L, Hypersensitivity reaction after inhalation of a lactose-containing dry powder inhaler. The journal of pediatric pharmacology and therapeutics : JPPT : the official journal of PPAG. 2014 Jul;     [PubMed PMID: 25309152]
[7] Fluticasone propionate and fluticasone propionate/salmeterol multidose dry powder inhalers compared with placebo for persistent asthma., D Sher L,Yiu G,Sakov A,Liu S,F Caracta C,, Allergy and asthma proceedings, 2017 Jun 21     [PubMed PMID: 28639542]
[8] Skoner DP, Inhaled corticosteroids: Effects on growth and bone health. Annals of allergy, asthma     [PubMed PMID: 27979015]
[9] Manara A,Hantson P,Vanpee D,Thys F, Lactic acidosis following intentional overdose by inhalation of salmeterol and fluticasone. CJEM. 2012 Nov;     [PubMed PMID: 23131487]
[10] Alhussien AH,Alhedaithy RA,Alsaleh SA, Safety of intranasal corticosteroid sprays during pregnancy: an updated review. European archives of oto-rhino-laryngology : official journal of the European Federation of Oto-Rhino-Laryngological Societies (EUFOS) : affiliated with the German Society for Oto-Rhino-Laryngology - Head and Neck Surgery. 2018 Feb;     [PubMed PMID: 29164323]
[11] Bouwmeester C,Kraft J,Bungay KM, Optimizing inhaler use by pharmacist-provided education to community-dwelling elderly. Respiratory medicine. 2015 Oct;     [PubMed PMID: 26341546]
[12] Holm A,Dijkstra M,Kleinjan A,Severijnen LA,Boks S,Mulder P,Fokkens W, Fluticasone propionate aqueous nasal spray reduces inflammatory cells in unchallenged allergic nasal mucosa: effects of single allergen challenge. The Journal of allergy and clinical immunology. 2001 Apr;     [PubMed PMID: 11295650]